The chemical substance employed in the present invention was first synthesized by K. L. Howard, et al and reported in J. Org. Chem., Vol. 18, page 1484 (1953). The authors found that 1-(2-pyrimidinyl)piperazine did not possess useful analgesic or antiparasitic (antifilarial) activity.
In much the same fashion, 1-(2-pyrimidinyl)piperazine has been used as a chemical intermediate for the synthesis of compounds with biological activity in a number of instances as borne out by the following representative references:
1. Carenini, et al., Boll. Farm., 117, 33-42 (1978). PA1 2. Khot, et al., Chem. Abstr., 90:72148k, p. 514 (1979). PA1 3. Indian Drugs and Pharmaceuticals, Chem. Abstr. (Pat. Abstr.) 95:61854q, p. 686 (1981).
Utility of this compound and related analogs as chemical intermediates in the synthesis of compounds with tranquilizing activity was disclosed in Wu, et al, U.S. Pat. No. 3,717,634 patented Feb. 20, 1973; U.S. Pat. No. 3,907,801 patented Sept. 23, 1975; and Wu, et al, J. of Medicinal Chemistry, 15/5, 477-479 (1972). Although 1-(2-pyrimidinyl)piperazine was subjected to in-house testing utilizing the same biological assays employed to determine tranquilizing activity for the claimed compounds in the Wu, et al patents, no activity of this sort was shown to be associated with 1-(2-pyrimidinyl)piperazine itself.
In summary, while 1-(2-pyrimidinyl)piperazine (MJ 13653) has been found to be useful as an intermediate in the preparation of biologically active molecules, nonetheless, no significant biological activity has previously been associated with the compound itself prior to the present invention.